Table 1.

Clinical trial relevance

Kinase target(s)Antagonistic phosphataseDrugTrial phaseCancerTrial ID
Protein kinase inhibitors
 AKTGSK2110183Phase IISolid tumors, hematologic malignanciesNCT01531894
 AKTMK2206Phase IIRelapsed or refractory acute myeloid leukemiaNCT01253447
 mTORC1EverolimusPhase IIMelanomaNCT01960829
 mTORC1SirolimusPhase IIHepatocellular carcinomaNCT01374750
 mTORC1TemsirolimusPhase I/IIAdvanced cancersNCT00877773
 mTORC1/2INK128Phase IAdvanced nonhematologic malignanciesNCT01899053
 mTORC1/2PHLPP1/2OSI-027Phase ISolid tumor, lymphomaNCT00698253
 mTORC1/2AZD8055Phase IGlioblastoma multiforme, other brain tumorsNCT01316809
Lipid kinase inhibitors
 PI3KBAY80-6946Phase IINon-Hodgkin lymphomaNCT01660451
 PI3KBKM120Phase IIIMetastatic breast cancer HR+, HER2NCT01633060
 PI3KPTENCAL101Phase IIIChronic lymphocytic leukemiaNCT01659021
 PI3KGDC0941Phase IINon–small cell lung cancerNCT01493843
 PI3KIPI145Phase IIIndolent non-Hodgkin lymphomaNCT01882803
 PI3KXL147Phase I/IIBreast cancer, breast neoplasmsNCT01042925
Dual specificity inhibitors
 PI3KmTORC1/2BEZ235Phase IIPancreatic neuroendocrine tumors (pNET)NCT01628913
 PI3KmTORC1/2PTENBGT226Phase I/IIAdvanced breast cancerNCT00600275
 PI3KmTORC1/2PF04691502Phase IIEndometrial neoplasmsNCT01420081
 PI3KmTORC1/2PHLPP1/2PF05212384Phase IIMetastatic colorectal cancerNCT01925274
 PI3KmTORC1/2XL765Phase IGlioblastoma, astrocytomaNCT01240460

NOTE: Phosphatase status could be used for patient stratification into matching clinical trials. Current phase II/III trials against pathway targets at the lipid and/or protein level are listed. Phosphatases that are functionally supported by each approach are indicated in the relevant phosphatase column.